Synthesis, Biological Activity and Preliminary in Silico ADMET Screening of Polyamine Conjugates with Bicyclic Systems

Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry
Marta SzumilakAgnieszka W Piastowska-Ciesielska

Abstract

Polyamine conjugates with bicyclic terminal groups including quinazoline, naphthalene, quinoline, coumarine and indole have been obtained and their cytotoxic activity against PC-3, DU-145 and MCF-7 cell lines was evaluated in vitro. Their antiproliferative potential differed markedly and depended on both their chemical structure and the type of cancer cell line. Noncovalent DNA-binding properties of the most active compounds have been examined using ds-DNA thermal melting studies and topo I activity assay. The promising biological activity, DNA intercalative binding mode and favorable drug-like properties of bis(naphthalene-2-carboxamides) make them a good lead for further development of potential anticancer drugs.

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Citations

Nov 23, 2019·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Jing HeRen-Bing Shi

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Methods Mentioned

BETA
Profiler
column chromatography
electrophoresis

Software Mentioned

GraphPad
Percepta
Cary WinUV
GraphPad Prism
ACD

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